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Journal articles on the topic 'Derivatives of pyrimidine'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

Verma, Vishal, Chandra Prakash Joshi, Alka Agarwal, Sakshi Soni, and Udichi Kataria. "A Review on Pharmacological Aspects of Pyrimidine Derivatives." Journal of Drug Delivery and Therapeutics 10, no. 5 (2020): 358–61. http://dx.doi.org/10.22270/jddt.v10i5.4295.

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Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogens at positions 1 and 3 in the ring. Pyrimidines are typically synthesized by the “Principal Synthesis” involving cyclization of beta-dicarbonyl compounds with N-C-N compounds. Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidiones, and guanidines to give 2-aminopyrimidines are typical. Pyrimidines can be prepared via the biginelli reaction. Many other methods

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2

Hossain, M. I., and M. M. H. Bhuiyan. "Synthesis and Antimicrobial Activities of Some New Thieno and Furopyrimidine Derivatives." Journal of Scientific Research 1, no. 2 (2009): 317–25. http://dx.doi.org/10.3329/jsr.v1i2.2299.

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Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6 dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitril

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3

Dabaeva, V. V., M. R. Baghdasaryan, I. M. Barkhudaryants, E. G. Paronikyan, and Sh Sh Dashyan. "Synthesis of new fused 3(4)-substituted 11-furylthieno[3,2-<i>d</i>]pyrimidine derivatives." Журнал общей химии 93, no. 9 (2023): 1351–57. http://dx.doi.org/10.31857/s0044460x23090056.

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A method was developed for the synthesis of new fused 3-alkyl-substituted derivatives of thieno[3,2- d ]pyrimidin-4(3 H )-ones based on 11-(2-furyl)-8,8-dimethyl-7,10-dihydro-8 H -pyrano[3′′,4′′:5′,6′]pyrido[3′,2′:4,5]-thieno[3,2- d ]pyrimidin-4(3 H )-one via nucleophilic substitution in the pyrimidine ring. A series of fused 4-amino-substituted 11-furylthieno[3,2- d ]pyrimidine derivatives was also synthesized from the corresponding 4-chloro derivative.

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4

Sirakanyan, Spinelli, Geronikaki, et al. "Synthesis, Antitumor Activity, and Docking Analysis of New Pyrido[3’,2’:4,5]furo(thieno)[3,2-d]pyrimidin-8-amines." Molecules 24, no. 21 (2019): 3952. http://dx.doi.org/10.3390/molecules24213952.

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Continuing our research in the field of new heterocyclic compounds, herein we report on the synthesis and antitumor activity of new amino derivatives of pyrido[3’,2’:4,5](furo)thieno[3,2-d]pyrimidines as well as of two new heterocyclic systems: furo[2–e]imidazo[1,2-c]pyrimidine and furo[2,3-e]pyrimido[1,2-c]pyrimidine. Thus, by refluxing the 8-chloro derivatives of pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidines with various amines, the relevant pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidin-8-amines were obtained. Further, the cyclization of some amines under the action of phosphorus oxychlori

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5

SABIU RABILU ABDULLAHI, ABUBAKAR MUHD SHAFI’I, SAPNA RAGHAV, and MA’ARUF ABDULMUMIN MUHAMMAD. "Pyrimidine derivatives: Recent discoveries and development towards its medicinal impact." GSC Advanced Research and Reviews 20, no. 1 (2024): 114–28. http://dx.doi.org/10.30574/gscarr.2024.20.1.0248.

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Pyrimidine derivatives' many biological functions and possible therapeutic uses have attracted a lot of research in the field of medicinal chemistry. Recent developments in the synthesis, biological assessment, and therapeutic uses of molecules based on pyrimidines are highlighted in this review. The significance of pyrimidine derivatives in treating a range of ailments, including cancer, infectious diseases, and metabolic disorders, is discussed, along with innovative synthesis approaches and important pharmacological findings. In order to give a thorough picture of the present status of pyri

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6

SABIU, RABILU ABDULLAHI, MUHD SHAFI'I ABUBAKAR, RAGHAV SAPNA, and ABDULMUMIN MUHAMMAD MA'ARUF. "Pyrimidine derivatives: Recent discoveries and development towards its medicinal impact." GSC Biological and Pharmaceutical Sciences 20, no. 1 (2024): 114–28. https://doi.org/10.5281/zenodo.13640628.

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Pyrimidine derivatives' many biological functions and possible therapeutic uses have attracted a lot of research in the field of medicinal chemistry. Recent developments in the synthesis, biological assessment, and therapeutic uses of molecules based on pyrimidines are highlighted in this review. The significance of pyrimidine derivatives in treating a range of ailments, including cancer, infectious diseases, and metabolic disorders, is discussed, along with innovative synthesis approaches and important pharmacological findings. In order to give a thorough picture of the present status of pyri

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7

Sarwade, Prakash Pralhad, K. M. Srinandhinidevi, Kiran Dangwal, et al. "Role of Pyrimidine Derivatives in the Treatment of Cancer." Journal for Research in Applied Sciences and Biotechnology 3, no. 5 (2024): 181–93. http://dx.doi.org/10.55544/jrasb.3.5.19.

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The study of the chemistry of pyrimidines is contributing to the expansion of research into the therapeutic applications of these compounds. In the field of medicinal chemistry, the sheer number of pyrimidine synthesis methods and reactions that are available opens up a world of possibilities. These investigations have been inspired by the fact that pyrimidines can be used as building blocks for a wide variety of compounds that have a physiological effect. The pyrimidine ring and its fused derivatives, which include pyrazolo[3,4-d]pyrimidine, pyrido[2,3-d]pyrimidine, quinazoline, and furo[2,3-

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8

Harnden, MR, and DT Hurst. "The Chemistry of Pyrimidinethiols. III. The Synthesis of Some Substituted Pyrimidinthiols and Some Thiazolo[5,4-D]pyrimidines." Australian Journal of Chemistry 43, no. 1 (1990): 55. http://dx.doi.org/10.1071/ch9900055.

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The preparation of a number of pyrimidinethiols and (substituted) thiopyrimidines has been carried out. The reaction of 5-acetylamino-2-aminopyrimidine-4,6-diol with phosphorus penta -sulfide in pyridine gave 5-amino-2-methylthiazolo[5,4-d]pyrimidine-7-thiol which was used to prepare several additional novel pyrimidine derivatives. Hydrolysis of the 4-carboxymethylthio derivative by using 5M hydrochloric acid gave 2,5-diamino-6-mercaptopyrimidin-4-ol hy -drochloride whilst hydrolysis of 2-methyl-7-methylthiothiazolo[5,4-d]pyrimidin-5-amine gave the corresponding 4-hydroxy derivative. Several 4

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9

Solomyannyi, Roman, Sergii Slivchuk, Donald Smee, et al. "In vitro Activity of the Novel Pyrimidines and Their Condensed Derivatives Against Poliovirus." Current Bioactive Compounds 15, no. 5 (2019): 582–91. http://dx.doi.org/10.2174/1573407214666180720120509.

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Background: Substituted pyrimidine derivatives (non-nucleoside) are found to be associated with various biological activities. The various substituted pyrimidines are also having significant in vitro activity against different DNA and RNA viruses. The present study focuses on the anti-PV activity of new pyrimidines and their condensed derivatives. Methods: A series of novel pyrimidines and their condensed derivatives were synthesized and their structures were confirmed by spectral data. Their antiviral activities against poliovirus type 3 (PV-3) were evaluated in vitro. In cell culture, morpho

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10

Agarkov, Artem S., Dilyara O. Mingazhetdinova, Anna A. Nefedova, et al. "Synthesis and Structure of 6-Acetyl-2-Arylhydrazone Derivatives of Thiazolo[3,2-a]Pyrimidine." Organics 4, no. 3 (2023): 438–46. http://dx.doi.org/10.3390/org4030031.

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Triazolo[4,3-a]pyrimidine is one of the promising structural fragments for the development of drugs, including anticancer drugs. This work is devoted to the synthesis of a number of new 2-arylhydrazone derivatives of thiazolo[3,2-a]pyrimidine, which are synthetic precursors for triazolo[4,3-a]pyrimidines. The crystal structure of 6-acetyl-7-methyl-5-phenyl-2-(2-phenylhydrazineylidene)-5H-thiazolo[3,2-a]pyrimidin-3(2H)-one was established by SCXRD. In the reduction reaction of the compound, the following system was used: vanadium(V) oxide, and sodium borohydride in ethanol at room temperature,

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11

Yavolovskii, Arkadii, Araksia Davtian, Lidiya Grishchuk, et al. "AMINATION OF 2-(2-OXO-2-ARYLETHYLTHIO)-PYRIMIDIN-4(3H)-ONE DERIVATIVES USING THE SULFONATE METHOD." Ukrainian Chemistry Journal 89, no. 1 (2023): 60–67. http://dx.doi.org/10.33609/2708-129x.89.01.2023.60-67.

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A Derivatives of 2-thiouracil are characterized by wide spectrum of biological activity, which is characteristic of most representatives this heterocycles class. In particular, 2-(2-oxo-2-phenylethylthio)-pyrimidin-4(3H)-ones belong to the group of non-nucleoside inhibitors of HIV-1 reverse transcriptase. The antimalarial properties of 2-(2-oxo-2-phenylethylthio)-4-R-pyrimidine derivatives, which proved to be effective inhibitors of CIpP protease of Plasmodium falciparum, are being studied. Known examples of 2-(2-oxo-2-phenylethylthio)-pyrimidines modification at the "4" position of the he

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12

Pandhurnekar, Chandrashekhar P., Ekta M. Meshram, Himani N. Chopde, and Rameshkumar J. Batra. "Synthesis, Characterization, and Biological Activity of 4-(2-Hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols Derivatives." Organic Chemistry International 2013 (July 1, 2013): 1–10. http://dx.doi.org/10.1155/2013/582079.

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With the aim of synthesizing new heterocyclic compounds and exploring biological potency, new series of chalcones, that is, 3-(2-hydroxy-5-(aryl-diazenyl)phenyl)-1-(aryl)prop-2-en-1-one and their pyrimidine derivatives, that is, 4-(2-hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols were synthesized using different aromatic amines and salicylaldehyde as starting moieties. The structures of newly synthesized compounds were confirmed using different spectroscopic techniques such as IR, 1H-NMR, 13C-NMR, and mass spectral analysis, and elemental analysis. The newly synthesized pyrimidines d

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13

Hussein, Khlood Abdulla Ahmed, and Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine." University of Aden Journal of Natural and Applied Sciences 25, no. 2 (2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted

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14

Hussein, Khlood Abdulla Ahmed, and Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine." University of Aden Journal of Natural and Applied Sciences 25, no. 2 (2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted

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15

Dawood, Dina H., Eman M. H. Abbas, Thoraya A. Farghaly, Mamdouh M. Ali, and Mohammed F. Ibrahim. "ZnO Nanoparticles Catalyst in the Synthesis of Bioactive Fused Pyrimidines as Anti-breast Cancer Agents Targeting VEGFR-2." Medicinal Chemistry 15, no. 3 (2019): 277–86. http://dx.doi.org/10.2174/1573406414666180912113226.

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Background: Pyrimidines emerged as a remarkable class of heterocyclic compounds that have reinforced the pharmaceutical chemistry with various bioactive antitumor agents. Moreover, pyrimidine scaffold displayed VEGFR-2 inhibitory activity. Also, nano-sized catalysts are used in organic reactions in order to speed up the catalytic process. Objective: We were interested herein to synthesize a new series of fused pyrimidines using ZnO(NPs) to investigate their antitumor efficiency against breast MCF7 cancer and their VEGFR- 2 inhibition properties. Method: A simple and efficient method for the sy

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16

Huppatz, JL. "Systemic Fungicides. The Synthesis of Pyrazolo[1,5-a]pyrimidine Analogues of Carboxin." Australian Journal of Chemistry 38, no. 1 (1985): 221. http://dx.doi.org/10.1071/ch9850221.

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The synthesis of a series of pyrazolo [1,5-a] pyrimidine derivatives, structural analogues of the systemic fungicide carboxin, is described. A common intermediate incorporating structural features desirable for fungicidal activity, N-phenyl-3(5)-amino-5(3)-methylpyrazole-4- carboxamide (6), was used to prepare pyrazolo [1,5-a] pyrimidines variously substituted in positions 5 and 7 of the ring system. Bromination of N-phenyl-2-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide (8) occurred preferentially in the phenyl ring and the 6-bromo derivative was prepared by bromination of the corresponding 3

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17

Edrees, Mastoura M. "Synthesis of 4-hydrazinopyrazolo[3,4-d]pyrimidines and their Reactions with Carbonyl Compounds." Journal of Chemical Research 37, no. 1 (2013): 6–10. http://dx.doi.org/10.3184/174751912x13543818811749.

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Synthesis of a new 4-hydrazinopyrazolo[3,4- d]pyrimidine was achieved via heating (4,6-dithioxo-1 H-pyrazolo[3,4- d] pyrimidin-3-yl)acetonitrile with hydrazine hydrate. Reactions of the latter product with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues afforded the corresponding hydrazone and pyrazole derivatives, respectively. Similarly, condensation of 2-[6-(benzylsulfanyl)-4-hydrazino-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues gave the respective hydrazone and pyrazolone derivatives. Alkylation

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18

Wenska, Grazyna, Bohdan Skalski, Stefan Paszyc, and Zofia Gdaniec. "Photochemistry of N-(pyrimidin-2-one-4-yl)pyridinium derivatives. The ring contraction of pyrimidinone into imidazolinone." Canadian Journal of Chemistry 73, no. 12 (1995): 2178–84. http://dx.doi.org/10.1139/v95-270.

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Photochemical reactions (λ > 300 nm) of N-(1-methylpyrimidin-2-one)-and N-(1,5-dimethyl-pyrimidin-2-one)pyridinium chlorides were studied in deoxygenated aqueous solution at various pH's. Only the former compound was found to be reactive under these conditions to give pyrimidine ring contraction photoproducts 1-methyl-4-imidazolin-2-one and 1-methyl-4-imidazolin-2-one-5-carboxyaldehyde, with pH-dependent chemical yields. The photochemical pyrimidine ring contraction reaction does not occur for other photochemically reactive pyrimidin-2-ones bearing 3-methylimidazolium-1,1,2,4-triazol-1-yl,

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19

Pathak, Archana, and Mahendra Kumar. "Synthesis and Biological Significance of Pyrimidine Derivatives as New Anti-bacterial Agents." Scientific Temper 13, no. 02 (2022): 208–16. http://dx.doi.org/10.58414/scientifictemper.2022.13.2.32.

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A heterocyclic moiety has great biological and medicinal significance. The variouspharmacological activities discussed here proves biological importance of pyrimidinemoietyAmong the diverse biological activities of pyrimidine derivatives are antiviral,anticancer, antifungal, antimalarial, sedative, hypnotic, anticonvulsant, anthelmintic, andantithyroid properties. The present research aims to focus on account of important chemicalmoiety, various derivatives of pyrimidine and its as antimicrobial agents. In the current studieswe synthesize pyrimidines derivatives derivatives and in vitro antimi

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20

SB, Patil. "Anticancer Potential of Novel Pyrimidine Analogs: Recent Updates." Medicinal and Analytical Chemistry International Journal 8, no. 1 (2024): 1–6. http://dx.doi.org/10.23880/macij-16000189.

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Pyrimidine, having two nitrogen atoms, looks like pyridine and benzene. In nature, pyrimidine is present in different forms, such as the bases of DNA and RNA. Due to its structure, various kinds of biological activity have been observed. The substituted and fused pyrimidine derivatives were chemically synthesized and showed anti-cancer potential against cancer cell lines (SW480, A549, CCRF-CEM, THP-1, HepG2, HCT-116, PC3, Huh-7, CNE-2, MGC-803, and MDA-MB-435). Based on the experimental results, the substituted pyrimidines and fused derivatives showed remarkably enhanced anticancer activity, w

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21

Tank, Manishkumar Jinabhai, Navinkumar A. Kucha, Chirag G. Naik, Tina R. Barot, and G. M. Malik. "Adamantane-pyrido[2,3-d]pyrimidine Derivatives; Synthesis, Characterization and Investigation of Antimicrobial Study." Oriental Journal Of Chemistry 39, no. 2 (2023): 393–402. http://dx.doi.org/10.13005/ojc/390219.

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Target molecules based on Adamantane-pyrido[2,3-d]pyrimidine derivatives were prepared. Adamantane-pyrido[2,3-d]pyrimidine series using N-(hydroxyadamantan-1-yl)-5-(2,4-substitutedphenyl)-2-Methyl-4-Oxo-7-(2-oxo-2H-Chromen-3-yl)pyrido[2,3-d]Pyrimidine-3(4H)carboxamide (6a-j) was synthesized by reaction between 3-(2-chloroacetyl)-5-(2,4-substitutedphenyl)-2-Methyl-7-(2-Oxo-2H-Chromen-3-yl) pyrido[2,3-d]pyrimidin-4(3H)-one (5a-j) and 3-aminoadamantan-1-ol. These derivatives of Adamantane-pyrido[2,3-d]Pyrimidine were investigated in vitro for their biological characteristics against the strains w

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22

Abdelhamid, Abdou O., Zeineb H. Ismail, and Anhar Abdel-Aziem. "Reactions with Hydrazonoyl Halides 601: Synthesis of Thieno[2′,3′:4,5] Pyrimidino[1,2-b][1,2,4,5]tetrazines, [1]benzothieno[2′,3′:4,5]pyrimidino [1,2-b][1,2,4,5]tetrazines, Pyrazolo[3′,4′:4,5]pyrimidino[1,2-b] [1,2,4,5]tetrazines and Pyrazolo[3,4-d]pyridazines." Journal of Chemical Research 2007, no. 10 (2007): 609–16. http://dx.doi.org/10.3184/030823407x256118.

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Thieno[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, [1]benzothieno-[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, pyrazolo [3′,4′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, triazolo[4,3- a]pyrimidin-5(1 H)-one, 1-{[2-(1-benzofuran-2-yl)-5-phenyl-4,5-dihydro-1 H-pyrazol-1-yl]-4-substituted-1,3-thiazol-5-yl}-2-phenyldiazene, 3-acyl-4-(1-benzofuran-2-ylcarbonyl) pyrazole and pyrazolo[3,4- d]pyridazine derivatives could be obtained via reactions of hydrazonoyl halides with the appropriate pyrimidine-2-thione, 3-amino-5,6-dimethyl-2-sulfanylthieno[2,3- d]pyrimidin-4(3 H)-one, 5-amino-6-mercapto

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23

Murat Saracoglu, Murat Saracoglu, Zulbiye Kokbudak Zulbiye Kokbudak, and M. Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli. "Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives." Journal of the chemical society of pakistan 42, no. 5 (2020): 746. http://dx.doi.org/10.52568/000679.

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Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental

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24

Murat Saracoglu, Murat Saracoglu, Zulbiye Kokbudak Zulbiye Kokbudak, and M. Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli. "Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives." Journal of the chemical society of pakistan 42, no. 5 (2020): 746. http://dx.doi.org/10.52568/000679/jcsp/42.05.2020.

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Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental

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25

Kumar, Sanjiv, Aakash Deep, and Balasubramanian Narasimhan. "A Review on Synthesis, Anticancer and Antiviral Potentials of Pyrimidine Derivatives." Current Bioactive Compounds 15, no. 3 (2019): 289–303. http://dx.doi.org/10.2174/1573407214666180124160405.

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Background: Pyrimidine is the six membered heterocyclic aromatic compound similar to benzene and pyridine containing two nitrogen atoms at 1st and 3rd positions. Pyrimidine is present throughout nature in various forms and is the building blocks of numerous natural compounds from antibiotics to vitamins and liposacharides. The most commonly recognized pyrimidines are the bases of RNA and DNA, the most abundant being cytosine, thymine or uracil. Results: Pyrimidine is a core structure in a wide variety of compounds that exhibits significant biological activity and also plays an important role i

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26

El-Gazzar, Abdel-Rahman, Hoda Hussein, and Hend Hafez. "Synthesis and biological evaluation of thieno[2,3-d]pyrimidine derivatives for anti-inflammatory, analgesic and ulcerogenic activity." Acta Pharmaceutica 57, no. 4 (2007): 395–411. http://dx.doi.org/10.2478/v10007-007-0032-6.

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Synthesis and biological evaluation of thieno[2,3-d]pyrimidine derivatives for anti-inflammatory, analgesic and ulcerogenic activity5-Methyl-6-phenyl-2-thioxothieno[2,3-d]pyrimidone derivative (2) reacted with hydrazonoyl chloride derivatives to afford triazolothienopyrimidones4a-f.Also, acetone-1-(2-amino-5-isopropyl-thiophene-3-carbonitrile) (3) reacted with functional and bifunctional groups to yield the corresponding compounds5-11. The new products showed anti-inflammatory, analgesic, and ulcerogenic activities comparable to that of indomethacin and acetylsalicylic acid, respectively.

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27

Mosaad, Sayed Mohamed, Mohamed Awad Samir, Abdallah Abd El-tawab Neama, and Mohamed Ahmed Naglaa. "An overview on synthesis and biological activity of pyrimidines." World Journal of Advanced Research and Reviews 15, no. 1 (2022): 272–96. https://doi.org/10.5281/zenodo.7743045.

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Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 of the six membered ring show wide range of biological activities. Numerous methods for the synthesis of pyrimidine and their diverse reactions offer enormous scope in the field of medicinal chemistry. Pyrimidine possesses wide spectrum of biological activities including antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer, and anti-HIV activity. The present review attempts to give brief information about the synthesis and various biological ac

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Ogurtsov, Vladimir A., and Oleg A. Rakitin. "6-(Chloromethyl)-N,1-dimethyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine." Molbank 2021, no. 4 (2021): M1294. http://dx.doi.org/10.3390/m1294.

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Functionally 4,6-disubstituted 1H-pyrazolo[3,4-d]pyrimidines are important compounds with various pharmacological activities. 1-Substituted 4-chloro-6-(chloromethyl)-1H-pyrazolo[3,4-d]pyrimidines are practically unexplored derivatives in this series. In this paper, it was shown that the nucleophilic substitution of 4-Chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine with methylamine produced selectively 4-substituted product, 6-(chloromethyl)-N,1-dimethyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine. The structure of the synthesized compound was established by elemental analysis, high resol

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Hamama, Wafaa S., Mohamed A. Ismail, Hana’a A. Al-Saman, and Hanafi H. Zoorob. "Convenient Selective Synthesis of Substituted Pyrido[2,3-d]pyrimidones and Annulated Derivatives." Zeitschrift für Naturforschung B 62, no. 1 (2007): 104–10. http://dx.doi.org/10.1515/znb-2007-0115.

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The reaction of 6-aminouracil (1) with the appropriate α,β -unsaturated ketones, gave the corresponding pyrido[2,3-d]pyrimidin-2,4-diones 3, 6, 8 and 10, respectively. Treatment of 1 with salicylaldehyde, 6-carboethoxy-3,5-diphenyl-2-cyclohexenone (13) or 2,6- bis(phenylmethylidene)cyclohexanone (15) afforded the corresponding pyrimido[4,5-d]quinoline- 2,4-diones 12, 14 and 16, respectively. Furthermore, a pyrido[2,3-d]pyrimidine incorporating 3,2’- bis(quinoline) derivative 18 was synthesized. Annulation of pyrido[2,3-d]pyrimidine with pyrazole or imidazole moieties was achieved via reaction

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A-Ani, Zaid S. M., Sana A. Abdulmawjood, Adel O. A. Al-Hussain, and Shihab A. Al-Bajari. "Synthesis and Biological Activity of few Pyrimidines Derivatives against Hepatic Injury Stimulated by Carbon Tetrachloride in Male Rats." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 12, no. 04 (2022): 1496–501. http://dx.doi.org/10.25258/ijddt.12.4.02.

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In the presence of sodium hydroxide, substituted chalcones are reacted with cyanoguandine in ethanol, and some chalcone compounds are used as a nucleus in the preparation of some five-, hexa-, and hepta-, heterocyclic compounds pyrimidine (pyrimidines derivatives), pyrimidine derivatives (A1, A2, and A3). Contains therapeutic properties and bioactivity, and has been used to treat various ailments. This study aimed to learn more about how pyrimidine derivatives could help mitigate the undesirable implications of carbon tetrachloride. a group of 50 male rats were separated into 5 groups: healthy

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Ho, Yuh-Wen, and Maw Cherng Suen. "Thioxopyrimidine in Heterocyclic Synthesis I: Synthesis of Some Novel 6-(Heteroatom-substituted)-(thio)pyrimidine Derivatives." Journal of Chemistry 2013 (2013): 1–15. http://dx.doi.org/10.1155/2013/765243.

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A series of novel N-cycloalkanes, morpholine, piperazines, pyrazole, pyrimidine, benzimidazolo[1,2-a]pyrimidine, 1,2,3,4-tetrazolo[1,5-a]pyrimidine, azopyrazolo[1,5- a]pyrimidine, pyrimido[4', 5':3,4]pyrazolo[1,5-a]pyrimidines and pyridine derivatives incorporating a 5-cyano-4-methyl-2-phenyl-(thio)pyrimidine moiety were obtained by the intramolecular cyclization of 6-methylthio-pyrimidine, 6-(benzoylmethyl)thio- pyrimidine and 2-[(5-cyano-4-methyl-2-phenylpyrimidin-6-yl)thio]-3-dimethyl- amino-1-phenyl-prop-2-en-1-one with appropriate amines and enaminone compounds, respectively. The structur

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Journal, Baghdad Science. "Synthesis of Some Heterocyclic Compounds derived from 2-mercapto pyrimidine." Baghdad Science Journal 7, no. 2 (2010): 1014–22. http://dx.doi.org/10.21123/bsj.7.2.1014-1022.

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In this work 2-hydrazino pyrimidine (1) was prepared from 2-mercapto pyrimidine with hydrazine hydrate. Treatment of (1) with active methylene compounds gave 2-(3,5-dimethyl -1 H – Pyrazole-1-yl) pyrimidine , whereas the reaction of (1) with carboxylic anhydride namely maleic anhydride or 1,2,3,6-tetra hydro phthalic anhydride yielded 1-Pyrimidine-2-yl-1,2-dihydro pyridazine-3,6-dione (3) and 2 – Pyrimidin -2-yl -2,3,4 a ,5,8 a – hexahydro phthalazine 1,4 – dione (4) . Reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-Phenyl-1,3-thiazolidine-2,4-dione-2( pyrimidine

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Askar, Firyal w., Huda A. Hassan, and Nahida A. Jinzeel. "Synthesis of Some Heterocyclic Compounds derived from 2-mercapto pyrimidine." Baghdad Science Journal 7, no. 2 (2010): 1014–22. http://dx.doi.org/10.21123/bsj.2010.7.2.1014-1022.

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In this work 2-hydrazino pyrimidine (1) was prepared from 2-mercapto pyrimidine with hydrazine hydrate. Treatment of (1) with active methylene compounds gave 2-(3,5-dimethyl -1 H – Pyrazole-1-yl) pyrimidine , whereas the reaction of (1) with carboxylic anhydride namely maleic anhydride or 1,2,3,6-tetra hydro phthalic anhydride yielded 1-Pyrimidine-2-yl-1,2-dihydro pyridazine-3,6-dione (3) and 2 – Pyrimidin -2-yl -2,3,4 a ,5,8 a – hexahydro phthalazine 1,4 – dione (4) . Reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-Phenyl-1,3-thiazolidine-2,4-dione-2( pyrimidine

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Nerkar, A. G., S. A. Ghone, and A. K. Thaker. "In SilicoScreening of the Library of Pyrimidine Derivatives as Thymidylate Synthase Inhibitors for Anticancer Activity." E-Journal of Chemistry 6, no. 3 (2009): 665–72. http://dx.doi.org/10.1155/2009/352717.

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We here report the virtual screening of several series of pyrimidine derivatives forin silicoThymidylate Synthase (TS) inhibition to arrive at possible potential inhibitors of TS with acceptable pharmacokinetic or ADME (Absorption, Distribution, Metabolism and Excretion) properties. Library of the molecules was constructed based upon structural modifications of pyrimidines nucleus. Structural modifications in descending order were performed for the series of pyrimidines,vizfrom pyrimidines with five membered heterocyclic ring to pyrimidines with four membered heterocyclic ring to simple pyrimi

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Sri Laya A, Govindarao Kamala, Tulasi K, et al. "Current Advances in Synthesis and Therapeutic Applications of Pyrimidine." Journal of Pharma Insights and Research 2, no. 6 (2024): 098–106. https://doi.org/10.69613/v6h5tv11.

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Pyrimidine derivatives are fundamental heterocyclic compounds that serve as essential components of nucleic acids, including uracil, thymine, and cytosine. Modern synthetic approaches for functionalized pyrimidines encompass metal-catalyzed reactions, multicomponent coupling strategies, and green chemistry protocols. The biological significance of pyrimidine scaffolds has led to numerous therapeutic applications across multiple disease states. Pyrimidine-based drugs demonstrate potent antimicrobial effects through antifolate mechanisms, as seen with trimethoprim and pyrimethamine. In antiviral

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Mamaghani, M., K. Tabatabaeian, R. Araghi, A. Fallah, and R. Hossein Nia. "An Efficient, Clean, and Catalyst-Free Synthesis of Fused Pyrimidines Using Sonochemistry." Organic Chemistry International 2014 (November 16, 2014): 1–9. http://dx.doi.org/10.1155/2014/406869.

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In this report, synthesis of indenopyrido[2,3-d]pyrimidine and pyrimido[4,5-b]quinoline derivatives was investigated via one-pot three-component reaction between 6-amino-2-(alkylthio)-pyrimidin-4(3H)one, 1,3-indanedione, or 1,3-cyclohexadione and arylaldehyde under ultrasonic irradiation in ethylene glycol as solvent at 65°C. In these reactions fused pyrimidine derivatives were synthesized with high to excellent yields (82–97%) and short reaction times (10–33 min).

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Azam, Mohammed Afzal, Loganathan Dharanya, Charu Chandrakant Mehta, and Sumit Sachdeva. "Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system." Acta Pharmaceutica 63, no. 1 (2013): 19–30. http://dx.doi.org/10.2478/acph-2013-0001.

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In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeru

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Ahmed Elkanzi, Nadia Ali. "Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review." Oriental Journal Of Chemistry 36, no. 6 (2020): 1001–15. http://dx.doi.org/10.13005/ojc/360602.

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Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and

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Mohamed, Mosaad, Ramdan El-Domany, and Rania Abd El-Hameed. "Synthesis of certain pyrrole derivatives as antimicro-bial agents." Acta Pharmaceutica 59, no. 2 (2009): 145–58. http://dx.doi.org/10.2478/v10007-009-0016-9.

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Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds

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40

Venugopala, Katharigatta N., and Vinuta Kamat. "Pyrimidines: A New Versatile Molecule in the Drug Development Field, Scope, and Future Aspects." Pharmaceuticals 17, no. 10 (2024): 1258. http://dx.doi.org/10.3390/ph17101258.

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Pyrimidine is a moiety that occurs in living organisms and has a variety of significant biological properties in pharmacology. Due to the easy handling of synthesis, easily available precursor, and less duration for the reaction, for the synthesis, not many technical skills are needed. All these factors attract chemists to focus more on pyrimidines. Apart from the synthesis of biological applications of pyrimidines, medicinal chemists have gathered to explore more pyrimidine scaffolds due to their interesting medicinal properties and easy targeting of various binding sites. This review delves

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Shevchenko, Nadiya М., Oleksandr O. Severin, Maryna V. Kachaeva, Oleksandr Р. Kozachenko, Yevheniia S. Velihina, and Volodymyr S. Brovarets. "Synthesis of new pyrrolo[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives of piperazin-1-yl-1,3-oxazole-4-carbonitriles, prediction and evaluation of their ADMET properties." Ukrainica Bioorganica Acta 19, no. 2 (2024): 21–32. https://doi.org/10.15407/bioorganica2024.02.021.

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The discovery of nucleoside antibiotics gave impetus to the development of the chemistry of pyrrolo[2,3-d]pyrimidines and thieno[2,3-d]pyrimidines as biologically active compounds. This work describes a universal and efficient approach to the synthesis of new pyrrolo[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives of piperazin-1-yl-1,3-oxazole-4-carbonitriles. Their potential as biologically active compounds is considered and ADMET-score is predicted to assess their further application as pharmaceutical substances

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42

Fawzy, Abdelshafy, M. Barqi Mashael, Ashar Ambreen, Javed Maria, Kanwal Ayesha, and R. Eletmany Mohamed. "Comprehensive Investigation of Pyrimidine Synthesis, Reactions, and Biological Activity." Comprehensive Investigation of Pyrimidine Synthesis, Reactions, and Biological Activity 8, no. 10 (2023): 21. https://doi.org/10.5281/zenodo.10049953.

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Researchers have devoted much attention to the study of the chemistry of pyrimidines due to their broad range of pharmaceutical activities. The important role of pyrimidines in the field of drugs is derived from the fact that they are present in genetic material of cells. In this review, we discuss various synthetic methods for pyrimidine derivatives, as well as their various categories of reactions and biological activities as illustrated by research conducted in recent years.Keywords:- Pyrimidine; Pharmaceutical Activities; Drugs.

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43

Swelam, Samira, Abd El-Salam, and Magdi Zaki. "Synthesis of some pyrazolo[3,4-d]pyrimidines and their fused triazole and tetrazole derivatives." Journal of the Serbian Chemical Society 64, no. 11 (1999): 655–62. http://dx.doi.org/10.2298/jsc9911655s.

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Reaction of 2 with different reagents, namely formic acid, acetic anhydride and trichloroacetonitrile, yielded pyrazolo[3,4-d]pyrimidine derivatives 3, 5 and 6, respectively. Pyrazolo[3,4-d]pyrimidine m-thiazine(7) and 2,4-(1H,3H)dithione (8) derivatives were formed by the action of carbon disulfide on 2, depending on the reaction medium. Interaction of 7 with hydrazine hydrate yielded the aminoimino derivative 9 which reacted with acetic anhydride, triethyl orthoacetate and/or appropriate aldehydes to give 11, 12 and 13a,b, respectively. Methylation of compound 8 gave 14, which reacted with h

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44

El-Nabi, Hisham A. Abd, A. M. Nour El-Din, and Magda S. Fahmi. "Synthesis of Functionalised Pyrimidin-2-One Derivatives." Journal of Chemical Research 2003, no. 8 (2003): 514–15. http://dx.doi.org/10.3184/030823403103174768.

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Pyrimidin-2-one and pyrimidine-2-thione derivatives 5 and 7 are obtained in 40-65% and 60-75% yields when 4-ethoxycarbonyl-5-phenylfuran-2,3-dione (1) react with semicarbazones, thiosemicarbazones 2a–f, urea and thiourea derivatives 6a–d through loss of water and carbon dioxide.

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45

Chandrani, Jeenkal P., and Kalpesh J. Ganatra. "An Efficient And Catalytically Free Chemical Transformation of Pyrimidin-2(1H)-one to 2-(N-Arylamino)pyrimidines and their in vitro Cytotoxicity Evaluation." Asian Journal of Organic & Medicinal Chemistry 5, no. 2 (2020): 133–37. http://dx.doi.org/10.14233/ajomc.2020.ajomc-p260.

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With the aim to develop an efficient strategy to synthesize pyrimidine derivatives bearing diversely substituted amines involves four step linear protocols started with Biginelli multi-component reaction leading to dihydropyrimidines which passing throug multistep sequantial process containing oxidation, chlorination and catalytically free transformation of pyrimidin-2(1H)-one to 2-(N-arylamino)pyrimidines, were evaluated for cytotoxicity study against human cancer lines HCT-116, Hep-G2 and QG-56. Compound 4j exhibit significant anticancer activity showed against: human hepato carcinoma (Hep-G

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46

Mamaghani, Manouchehr. "Ultrasound-promoted synthesis of novel dihydropyrido[2,3-d:5,6- d`]dipyrimidine derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 11, no. 5 (2015): 3567–75. http://dx.doi.org/10.24297/jac.v11i5.4475.

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An efficient synthesis of dihydropyrido[2,3-d:5,6-d`]pyrimidine derivatives was developed via one-pot three-component reaction of 6-amino-2-(alkylthio)-pyrimidine-4(3H)one and aryl aldehydes in the mixed solvent of glacial acetic acid and DMF (1:1, v:v) under ultrasonic irradiation. In this protocol novel fused dihydropyrido[2,3-d]pyrimidines were synthesized in high yields (80-97%) and lower reaction times (5-25 min).

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47

Mosaad Sayed Mohamed, Samir Mohamed Awad, Neama Abdallah Abd El-tawab, and Naglaa Mohamed Ahmed. "An overview on synthesis and biological activity of pyrimidines." World Journal of Advanced Research and Reviews 15, no. 1 (2022): 272–96. http://dx.doi.org/10.30574/wjarr.2022.15.1.0689.

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Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 of the six membered ring show wide range of biological activities. Numerous methods for the synthesis of pyrimidine and their diverse reactions offer enormous scope in the field of medicinal chemistry. Pyrimidine possesses wide spectrum of biological activities including antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer, and anti-HIV activity. The present review attempts to give brief information about the synthesis and various biological ac

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48

Tomé, Augusto C., Roger F. Enes, José A. S. Cavaleiro*, and José Elguero. "Pyrimidine and Pyrimidone Derivatives of [60]Fullerene." Tetrahedron Letters 38, no. 14 (1997): 2557–60. http://dx.doi.org/10.1016/s0040-4039(97)00400-0.

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49

Velihina, Y. S., S. G. Pilyo, I. V. Ivanova, and V. S. Brovarets. "Synthesis of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives and study of their vasodilator activity." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 2 (May 2023): 51–60. http://dx.doi.org/10.32434/0321-4095-2023-147-2-51-60.

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A number of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives were synthesized and characterized. Pyrazolo[1,5-a][1,3,5]triazines with various substituents in the fourth position and a dichloromethyl group in the second position were obtained by the heterocyclization reaction of available N-(2,2-dichloro-1-cyanoethenyl)carboxamides and 5-aminopyrazoles. Oxazolo[4,5-d]pyrimidines were obtained by treating 2-phenyl-4-dichloromethylene-1,3-oxazol-5(4H)-one with the corresponding arylamidine hydrochloride in the presence of triethylamine. The resulting 4,5-dihydro-1H-imidazol

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50

Povidaichyk, M., О. Onysko, and M. Onysko. "SYNTHESIS OF TERMINAL 2-ALKENYL(ALKYNYL)THIO-5-CYANO-6-(p-DIMETHYLAMINOPHENYL)PYRIMIDIN-4-ONES." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 48, no. 2 (2023): 79–83. http://dx.doi.org/10.24144/2414-0260.2022.2.79-83.

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Functionalized pyrimidines possess a wide spectrum of biological activity. In particular, they have antitumor, antiviral, and anticonvulsant activities, exhibit anti-inflammatory and analgesic effects, and they are inhibitors of aldose reductase, SecA ATPase, azide, and plant growth. The search for methods of synthesis of new functionalized and condensed pyrimidine derivatives is an urgent problem. Alkenyl-functionalized mono- and polycyclic pyrimidines are promise substrates for studying the regioselectivity of electroph ilic heterocyclization reactions under the influence of halogen-co

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